Adrenergic Agonists- T2 Flashcards
define asthma
increased inflammation and contractile responsiveness of bronchial smooth muscle in response to allergens, pollutants, exercise and upper respiratory infections.
4 structure examples given of beta2 adrenergic agonists
albuterol, metaproterenol, terbutaline, and formoterol.
beta2 adrenergic agonists are suppled as ____ mixtures of R and S forms of the drug
racemic
Levalbuterol is which isomer?
R
which isomer is more efficacious and why is the other not as good
R. S tends to hang around longer making it more susceptible to metabolism and has a longer half life.
beta2 adrenoceptors predominate as the primary adrenergic receptor producing __
relaxation of bronchial smooth muscle.
activation of M3–> ___ –> —
increase Ca (PLC)–> increase bronchoconstriction
activation of B2–> ___ –> ___ –> ____
increase cAMP–> PKA –> decrease Ca
is beta2 selectivity absolute?
no, if you take enough, you can activate beta1.
what size particle is optimal for bronchial tree deposition
2-5 micrometers
systemic effects of beta agonists
skeletal muscle tremors, weakness, tachycardia, CNS excitation.
genetic studies have revealed that polymorphism in ____ may modify asthmatic disease or response
beta2 receptor
polymorphism is __ and mutation is ___
polymorph: greater than 1% and mutation is less than 1%
differences in ___ lead to differences in the ___
receptors, patients response to the drug
these polymorphisms change how the receptors react-
the beta receptors couple to cAMP production though a Gs, this cAMP buildup through PKA in the bronchioles is going to cause bronchiodilation, this is going to be caused by removal of Ca, ig we have a polymorph then the receptor doesn’t couple well to the G protein system so we reduce the ability for the receptor to cause bronchodilation.
